JG-98 是一种热休克蛋白 70(Hsp70)变构抑制剂，可与 Hsp70 上的保守位点紧密结合，打断 Hsp70-Bag3 相互作用。JG-98 影响癌细胞和肿瘤相关巨噬细胞，显示抗癌活性。
| 生物活性 | JG-98, an allostericheat shock protein70 (Hsp70)inhibitor, which binds tightly to a conserved site onHsp70and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities affecting bothcancercells and tumor-associated macrophages[1][2][3]. |
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体外研究
(In Vitro) | JG-98 (30 nM-30 μM; 72 hours) has antiproliferative activity across a range of cell lines with the EC50s between ~0.3 and 4 μM[2].
JG-98 (10 μM; 48 hours) activates apoptotic mediators (cleavage of caspase-3 and PARP) in MDA-MB-231 cells[1].
JG-98 destabilizes FoxM1 and relieves suppression of downstream effectors, including p21 and p27[2].
Cell Proliferation Assay[2] | Cell Line: | MCF-7, MDA-MB-231, A375, MeWo, HeLa, HT-29, SKOV3, Jurkat, mouse embryonic fibroblasts (MEF), MM1.R, INA6, RPMI-8226, JJN-3, U266, NCI-H929, L363, MM1.S, KMS11, LP-1, AMO-1, OPM1, OPM2 cells | | Concentration: | 30 nM-30 μM | | Incubation Time: | 72 hours | | Result: | Active against all of the lines tested, and the EC50s were variable (between ~0.3 μM and 4 μM). Normal MEFs and OPM1 and OPM2 were relatively less sensitive. |
Western Blot Analysis[1] | Cell Line: | MDA-MB-231 cells | | Concentration: | 10 μM | | Incubation Time: | 48 hours | | Result: | Incudes apoptotic mediators cleavage of caspase 3 and PARP. |
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体内研究
(In Vivo) | JG-98 (3 mg/kg; i.p.; on days 0, 2, and 4) suppresses tumor growth in xenograft models bearing MCF7 and HeLa cells[2].
| Animal Model: | 6-week-old NCR mice (xenografts of MCF7 and HeLa cells)[2] | | Dosage: | 3 mg/kg | | Administration: | Intraperitoneal injection; on days 0, 2, and 4 | | Result: | Limited tumor growth, but somewhat less effectively. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 5 mg/mL(9.35 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.8708 mL | 9.3538 mL | 18.7077 mL | | 5 mM | 0.3742 mL | 1.8708 mL | 3.7415 mL | | 10 mM | --- | --- | --- |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
